Identification | Back Directory | [Name]
NDT-19795 | [CAS]
2272917-12-9 | [Synonyms]
NDT-19795 2-Pyrimidinepropanoic acid, α-[[[(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)amino]carbonyl]oxy]-, (αR)- | [MOL File]
2272917-12-9.mol | [Molecular Weight]
367.4 |
Chemical Properties | Back Directory | [Boiling point ]
528.1±50.0 °C(predicted) | [density ]
1.401±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
2.37±0.10(predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
NDT-19795 is an effective inhibitor of the NLRP3 inflammasome with an IC50 value of 66 nM in the PBMC method and 4.7 μM in the WB method. NDT-19795 is a carboxylic acid-active substance that can be converted from NT-0796 (HY-156438) within cells. NDT-19795 can be used for the study of neurological diseases[1]. | [in vivo]
NDT-19795 (3 mg/kg; i.v.; single dose) exhibits a brain-to-blood ratio of 0.07 in C57BL/6 mice, indicating low permeability through the blood-brain barrier[1]. | [References]
[1] Harrison D, et al. Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders. J Med Chem. 2023;66(21):14897-14911. DOI:10.1021/acs.jmedchem.3c01398 |
|
|